Bupivacaine hydrochloride(Synonyms: 盐酸布比卡因)

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Bupivacaine hydrochloride (Synonyms: 盐酸布比卡因) 纯度: 99.41%

Bupivacaine hydrochloride 是一种 NMDA 受体抑制剂。Bupivacaine 可以阻断钠、L-钙和钾通道。Bupivacaine 有效阻断 SCN5A 通道，IC50 为 69.5 μM。Bupivacaine hydrochloride 可用于慢性疼痛的研究。

Bupivacaine hydrochloride(Synonyms: 盐酸布比卡因)

Bupivacaine hydrochloride Chemical Structure

CAS No. : 18010-40-7

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥790 In-stock
100 mg ￥600 In-stock
500 mg ￥900 In-stock
1 g   询价  
5 g   询价  

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生物活性

Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain[1][2][3].

IC50 & Target

Sodium Channel[1]
体外研究
(In Vitro)

Bupivacaine hydrochloride inhibits NMDA receptor-mediated synaptic transmission in the dorsal horn of the spinal cord, an area critically involved in central sensitization[1].
Bupivacaine hydrochloride influences the voltage dependency of channel activation and steady-state inactivation by shifting the membrane potential of half-maximal activation/inactivation toward somewhat more negative membrane potentials. In their inactivated state, SCN5A channels are slightly sensitive toward Bupivacaine hydrochloride IC50=2.18±0.16 μM[2].
Bupivacaine hydrochloride reversibly inhibits the SK2 channel in a dose-dependent manner with the IC 50 of 16.5 µM[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: HEK 293 cells transfected with the SK2 gene (transfected cells were named SK2 cells)
Concentration: 10, 100, 1000 µM
Incubation Time:
Result: The IC50 value was 16.5 µM.

Clinical Trial

分子量

324.89

Formula

C18H29ClN2O
CAS 号

18010-40-7
中文名称

盐酸布比卡因
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (76.95 mM; Need ultrasonic)

H2O : 12.5 mg/mL (38.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0780 mL 15.3898 mL 30.7796 mL
5 mM 0.6156 mL 3.0780 mL 6.1559 mL
10 mM 0.3078 mL 1.5390 mL 3.0780 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： PBS

    Solubility: 13 mg/mL (40.01 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.69 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.69 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.69 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Casati A, et, al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):247-68.

    [2]. Dan J, et, al. Inhibition of gastric cancer by local anesthetic bupivacaine through multiple mechanisms independent of sodium channel blockade. Biomed Pharmacother. 2018 Jul;103:823-828.

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